Nurses Compass
Drug Guide
Rolapitant Hydrochloride
Classification
Therapeutic: Antiemetic
Pharmacological: NK1 receptor antagonist
FDA Approved Indications
- Prevention of chemotherapy-induced nausea and vomiting (CINV)
Mechanism of Action
Rolapitant is a selective antagonist of the neurokinin-1 (NK1) receptor, blocking the action of substance P, a neuropeptide involved in nausea and vomiting pathways, thereby preventing CINV.
Dosage and Administration
Adult: 180 mg orally 2 hours prior to chemotherapy, then 90 mg once daily on days 2 and 3 if chemotherapy lasts longer.
Pediatric: Not approved for pediatric use.
Geriatric: No specific dosage adjustment; use with caution and monitor for side effects.
Renal Impairment: No specific adjustment recommended.
Hepatic Impairment: Use with caution; no specific dose adjustment recommended.
Pharmacokinetics
Absorption: Well absorbed orally.
Distribution: High protein binding (~99%).
Metabolism: Metabolized primarily via CYP3A4, CYP1A2, and CYP2D6.
Excretion: Primarily fecal and renal excretion of metabolites.
Half Life: Approximately 7-9 days.
Contraindications
- Hypersensitivity to rolapitant or any component of the formulation.
Precautions
- Use with caution in patients taking drugs that prolong QT interval; monitor cardiac function as needed.
- Alcohol can increase blood levels of the drug; advise moderation or avoidance.
Adverse Reactions - Common
- Fatigue (Unknown)
- Hiccups (Unknown)
- Decreased appetite (Unknown)
- Constipation (Unknown)
Adverse Reactions - Serious
- Serious hypersensitivity reactions (Rare)
- QT prolongation leading to arrhythmias (Rare)
Drug-Drug Interactions
- Potential interactions with drugs that are CYP3A4 inhibitors or inducers; may increase or decrease effectiveness of other drugs.
Drug-Food Interactions
- Avoid alcohol during treatment due to potential increase in blood levels.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Assess patient for history of QT prolongation, electrolyte imbalance, or hypersensitivity.
Diagnoses:
- Risk for nausea related to chemotherapy.
- Risk for cardiac arrhythmias related to QT prolongation.
Implementation: Administer as prescribed prior to chemotherapy. Monitor cardiac status as indicated.
Evaluation: Evaluate effectiveness in preventing nausea and monitoring for adverse effects.
Patient/Family Teaching
- Take medication exactly as prescribed, including timing.
- Report any signs of allergic reactions or irregular heartbeat.
- Limit alcohol consumption during therapy.
- Understand that this medication helps prevent nausea associated with chemotherapy.
Special Considerations
Black Box Warnings:
- QT prolongation and arrhythmias, including torsades de pointes. Use with caution in patients with a history of arrhythmias or electrolyte disturbances.
Genetic Factors: CYP3A4 polymorphisms may influence metabolism.
Lab Test Interference: May interfere with CYP3A4 substrates testing.
Overdose Management
Signs/Symptoms: Nausea, vomiting, dizziness, arrhythmias.
Treatment: Supportive care, monitored cardiac assessment, activated charcoal if ingestion is recent.
Storage and Handling
Storage: Store at room temperature away from light and moisture.
Stability: Stable under recommended conditions for the shelf life as indicated on the package.